Abstract:
:Novel primaquine-cell penetrating peptide conjugates were synthesised and tested in vitro against liver stage Plasmodium berghei parasites. Generally, the conjugates were more active than the parent peptides and, in some cases, than the parent drug. These are unprecedented findings that may open a new route towards antimalarial drug rescuing.
journal_name
Medchemcommjournal_title
MedChemCommauthors
Aguiar L,Machado M,Sanches-Vaz M,Prudêncio M,Vale N,Gomes Pdoi
10.1039/c8md00447asubject
Has Abstractpub_date
2018-11-16 00:00:00pages
221-226issue
2eissn
2040-2503issn
2040-2511pii
c8md00447ajournal_volume
10pub_type
杂志文章相关文献
MedChemComm文献大全abstract::Receptor mediated gene delivery to the liver offers advantages in treating genetic disorders such as hemophilia and hereditary tyrosinemia type I (HTI). Prior findings demonstrated that tethering the d-galactose head group to cationic lipids directs genes to the liver via asialoglycoprotein receptors (ASGPRs). In our ...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c7md00503b
更新日期:2017-12-06 00:00:00
abstract::Phenotypic screening is in a renaissance phase and is expected by many academic and industry leaders to accelerate the discovery of new drugs for new biology. Given that phenotypic screening is per definition target agnostic, the emphasis of in silico and in vitro follow-up work is on the exploration of possible molec...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c6md00065g
更新日期:2016-06-01 00:00:00
abstract::N-Acylethanolamine acid amidase (NAAA) is one of the key enzymes involved in the degradation of fatty acid ethanolamides (FAEs), especially for palmitoylethanolamide (PEA). Pharmacological blockage of NAAA restores PEA levels, providing therapeutic benefits in the management of inflammation and pain. In the current wo...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c8md00432c
更新日期:2018-12-18 00:00:00
abstract::In this review, we have focused on the recent progress in metal complexes that are able to bind to β-amyloid (Aβ) species. We have discussed various radioactive complexes of 99mTc, 68Ga, 64Cu, 89Zr, and 111In, which were designed as Aβ imaging agents for positron emission tomography (PET) and single photon emission co...
journal_title:MedChemComm
pub_type: 杂志文章,评审
doi:10.1039/c7md00064b
更新日期:2017-05-16 00:00:00
abstract::Periodontal disease is an oral chronic immune-inflammatory disease highly prevalent worldwide that is initiated by specific oral bacterial species leading to local and systemic effects. The development of new preventive/therapeutic strategies to specifically target oral periodontopathogens without perturbing oral micr...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c9md00074g
更新日期:2019-06-10 00:00:00
abstract::The benzophenone scaffold represents a ubiquitous structure in medicinal chemistry because it is found in several naturally occurring molecules which exhibit a variety of biological activities, such as anticancer, anti-inflammatory, antimicrobial, and antiviral. In addition, various synthetic benzophenone motifs are p...
journal_title:MedChemComm
pub_type: 杂志文章,评审
doi:10.1039/c8md00300a
更新日期:2018-08-23 00:00:00
abstract::As the protein databank (PDB) recently passed the cap of 123 456 structures, it stands more than ever as an important resource not only to analyze structural features of specific biological systems, but also to study the prevalence of structural patterns observed in a large body of unrelated structures, that may refle...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c7md00381a
更新日期:2017-10-01 00:00:00
abstract::Classical aminoglycoside antibiotics are obsolete or hampered by the emergence of drug resistant bacteria. Recent discoveries of antifungal amphiphilic kanamycins offer new strategies for reviving and repurposing these old drugs. A simple structural modification turns the clinically obsolete antibacterial kanamycin in...
journal_title:MedChemComm
pub_type: 杂志文章,评审
doi:10.1039/c8md00155c
更新日期:2018-04-17 00:00:00
abstract::Rigidification of the isobutyl side chain of drug-like AT2 receptor agonists and antagonists that are structurally related to the first reported selective AT2 receptor agonist 1 (C21) delivered bioactive indane derivatives. Four enantiomer pairs were synthesized and the enantiomers were isolated in an optical purity >...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c9md00402e
更新日期:2019-11-18 00:00:00
abstract::The dopamine D3 receptor (D3R) is a proven therapeutic target for the treatment of neurological and neuropsychiatric disorders. In particular, D3R-selective ligands that can eliminate side effects associated with dopamine D2 receptor (D2R) therapeutics have been validated. However, the high homology in signaling pathw...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c8md00237a
更新日期:2018-06-14 00:00:00
abstract::The dynamic and crucial role of tubulin in different cellular functions rendered it a promising target in anticancer drug development. Combretastatin A-4 (CA-4), an inhibitor of tubulin polymerization isolated from natural sources, is a lead molecule with significant cytotoxicity against tumour cells. Owing to its non...
journal_title:MedChemComm
pub_type: 杂志文章,评审
doi:10.1039/c7md00227k
更新日期:2017-07-04 00:00:00
abstract::Twenty-four 14-sulfonamide-tetrandrine derivatives as potential anti-cancer agents were synthesized. The synthetic derivatives were investigated for their cytotoxic activity against human cancer cell lines MDA-MB-231, PC3, WM9, HEL and K562. Initially, the IC50 values (50% inhibitory concentrations) of all of the comp...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c8md00125a
更新日期:2018-05-04 00:00:00
abstract::Diabetes mellitus is a chronic, complex and multifactorial disease associated characteristically with hyperglycemia. One of the most recently approved antidiabetic drug classes for clinical use are sodium-glucose cotransporter type 2 (SGLT-2) inhibitors. SGLT-2 is a protein expressed in the kidneys, responsible for gl...
journal_title:MedChemComm
pub_type: 杂志文章,评审
doi:10.1039/c8md00183a
更新日期:2018-06-06 00:00:00
abstract::A series of 4-thiazolidinone derivatives were synthesized and evaluated as novel human dihydroorotate dehydrogenase (hDHODH) inhibitors. Compounds 26 and 31 displayed IC50 values of 1.75 and 1.12 μM, respectively. The structure-activity relationship was summarized. Further binding mode analysis revealed that compound ...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c7md00081b
更新日期:2017-04-26 00:00:00
abstract::Twenty-three monoketone derivatives of curcumin were synthesized to investigate the synergy with fluconazole against fluconazole-resistant Candida spp. The minimal inhibitory concentration (MIC80) and the fractional inhibitory concentration index (FICI) of the antifungal synergist fluconazole were measured against flu...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c6md00649c
更新日期:2017-03-17 00:00:00
abstract::Three series of compounds were designed, synthesized and evaluated for their in vitro anticancer activity against a procaspase-3 over-expression cancer cell line (U937) and a procaspase-3 no-expression cancer cell line (MCF-7) to rule out off-target effects. Biological evaluation led to the identification of a series ...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c8md00624e
更新日期:2019-02-25 00:00:00
abstract::Tuberculosis (TB) is an epidemic disease and the growing burden of multidrug-resistant (MDR) TB world wide underlines the need to discover new drugs to treat the disease. Mycobacterium tuberculosis (Mtb) is the etiological agent of most cases of TB. Mtb is difficult to treat, in part, due to the presence of a sturdy h...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/C5MD00376H
更新日期:2016-01-01 00:00:00
abstract::Bile acids have emerged as strong signaling molecules capable of influencing various biological processes like inflammation, apoptosis, cancer progression and atherosclerosis depending on their chemistry. In the present study, we investigated the effect of major hydrophobic bile acids lithocholic acid (LCA) and deoxyc...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c7md00475c
更新日期:2017-10-31 00:00:00
abstract::Recent studies point towards the possible disadvantages of using hydroxamic acid-based zinc-binding groups in HDAC inhibitors due to e.g. mutagenicity issues. In this work, we elaborated on our previously developed Tubathian series, a class of highly selective thiaheterocyclic HDAC6 inhibitors, by replacing the benzoh...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c8md00107c
更新日期:2018-05-18 00:00:00
abstract::A focused library of 24 N-aryl urea derivatives was prepared and evaluated against serine esterases of Mycobacterium tuberculosis (Mtb) Rv3802c and Mtb Ag85C. The members of the library were evaluated for both selectivity and mode of inhibition. Furan-based urea derivative 6c was found to be the most potent non-covale...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c9md00122k
更新日期:2019-06-04 00:00:00
abstract::Porphyrins are tetrapyrrolic macrocyclic ligands known for their affinity towards neoplastic tissues and once radiolabeled with a suitable diagnostic radioisotope could potentially be used for the imaging of tumorous lesions. In the present study, an unsymmetrically substituted porphyrin derivative namely 5-(p-amino-p...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c8md00559a
更新日期:2019-02-22 00:00:00
abstract::A series of indole derivatives was designed and synthesised to improve on activity and circumvent pharmacokinetic limitations experienced with the structurally related compound, ladostigil. The compounds consisted of a propargylamine moiety (a known MAO inhibitor and neuroprotector) at the N1 position and a ChE inhibi...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c7md00569e
更新日期:2018-01-16 00:00:00
abstract::[This corrects the article DOI: 10.1039/C7MD00637C.]. ...
journal_title:MedChemComm
pub_type: 杂志文章,已发布勘误
doi:10.1039/c8md90009d
更新日期:2018-03-02 00:00:00
abstract::The development of novel nanoscale vehicles for drug delivery promotes the growth of interest in investigations of interaction between nanomaterials. In this paper, we report the in vitro studies of eukaryotic cell physiological response to incubation with graphene oxide and planar kaolin nanoclay. Graphene family mat...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c8md00633d
更新日期:2019-06-10 00:00:00
abstract::[This corrects the article DOI: 10.1039/C0MD00060D.]. ...
journal_title:MedChemComm
pub_type: 已发布勘误
doi:10.1039/c8md90010h
更新日期:2018-03-19 00:00:00
abstract::The type III secretion system injectisome is a syringe-like multimembrane spanning nanomachine that is essential to the pathogenicity but not viability of many clinically relevant Gram-negative bacteria, such as enteropathogenic Escherichia coli, Salmonella enterica and Pseudomonas aeruginosa. Due to the rise in antib...
journal_title:MedChemComm
pub_type: 杂志文章,评审
doi:10.1039/c9md00146h
更新日期:2019-06-20 00:00:00
abstract::A series of novel indazole-pyrone hybrids were synthesized by a one pot reaction between N-alkyl-6(5)-nitroindazoles and 2-pyrone (4-hydroxy-6-methyl-2H-pyran-2-one) using indium or stannous chloride as the reducing system in the presence of acetic acid in tetrahydrofuran. The hybrid molecules were obtained in good to...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c8md00475g
更新日期:2018-11-19 00:00:00
abstract::Recently, there has been an emergence of significant interest in silver-based antimicrobials. Our goal was to develop a radioactive tracer for investigating the biological fate of such compounds. Purified 111Ag was incorporated into the methylated caffeine analogue, IC1 to yield the silver carbene complex designated a...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/C3MD00082F
更新日期:2013-06-01 00:00:00
abstract::Many reports have suggested that NRP-1 acts as a co-receptor for VEGF-A165 and boosts tumour growth and metastasis. This NRP-1, due to its important role in tumour progression, triggered interest in the design of new molecules able to significantly inhibit NRP-1/VEGF-A165 interaction to suppress pathological angiogene...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c8md00537k
更新日期:2019-01-25 00:00:00
abstract::Fungal infections directly affect millions of people each year. In addition to the invasive fungal infections of humans, the plants and animals that comprise our primary food source are also susceptible to diseases caused by these eukaryotic microbes. The need for antifungals, not only for our medical needs, but also ...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/C6MD00222F
更新日期:2016-07-01 00:00:00